公开(公告)号：US07390809B2

公开(公告)日：2008-06-24

申请号：US10530215

申请日：2003-10-03

申请人： Dooseop Kim ,  Jennifer E. Kowalchick

发明人： Dooseop Kim ,  Jennifer E. Kowalchick

IPC分类号： C07D487/04 ,  A61K31/5025 ,  A61P3/10

CPC分类号： C07D487/04

摘要： The present invention is directed to compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）的抑制剂的结构式（I）的化合物，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及二肽基肽酶-IV酶的疾病中的用途

公开(公告)号：US08445480B2

公开(公告)日：2013-05-21

申请号：US12664757

申请日：2008-06-16

申请人： Julianne A. Hunt ,  Ramzi F. Sweis ,  Dooseop Kim ,  Florida Kallashi ,  Peter J. Sinclair

发明人： Julianne A. Hunt ,  Ramzi F. Sweis ,  Dooseop Kim ,  Florida Kallashi ,  Peter J. Sinclair

IPC分类号： A61K31/553 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/423 ,  A61K31/438 ,  C07D239/42 ,  C07D267/10 ,  C07D413/14 ,  C07D401/14 ,  C07D221/20 ,  C07D211/26 ,  C07D263/57

CPC分类号： C07D413/14 ,  C07D413/10 ,  C07D413/12

摘要： Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.

摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是有效的CETP（胆固醇酯转移蛋白）抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。动脉粥样硬化及其临床 后果，冠心病（CHD），中风和血管性血管疾病对工业化世界的保健系统来说是一个真正的巨大负担。在公式I中，AB是芳基酰胺部分。

公开(公告)号：US06498161B1

公开(公告)日：2002-12-24

申请号：US09543019

申请日：2000-04-04

申请人： Charles G. Caldwell ,  Kevin T. Chapman ,  Jeffrey Hale ,  Dooseop Kim ,  Christopher Lynch ,  Malcolm MacCoss ,  Sander G. Mills ,  Christopher Willoughby ,  Scott Berk ,  Ronald M. Kim

发明人： Charles G. Caldwell ,  Kevin T. Chapman ,  Jeffrey Hale ,  Dooseop Kim ,  Christopher Lynch ,  Malcolm MacCoss ,  Sander G. Mills ,  Christopher Willoughby ,  Scott Berk ,  Ronald M. Kim

IPC分类号： A61K31165

CPC分类号： C07D401/14 ,  C07D401/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/10 ,  C07F9/59 ,  C07F9/65583

摘要： The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

摘要翻译： 本发明涉及可用作趋化因子受体活性的调节剂的式I的吡咯烷化合物（其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所定义）。 特别地，这些化合物可用作趋化因子受体CCR-5和/或CCR-3的调节剂。

公开(公告)号：US06265434B1

公开(公告)日：2001-07-24

申请号：US09543024

申请日：2000-04-04

申请人： Charles Caldwell ,  Kevin T. Chapman ,  Jeffrey Hale ,  Dooseop Kim ,  Christopher Lynch ,  Malcolm MacCoss ,  Sander G. Mills ,  Keith Rosauer ,  Christopher Willoughby ,  Scott Berk

发明人： Charles Caldwell ,  Kevin T. Chapman ,  Jeffrey Hale ,  Dooseop Kim ,  Christopher Lynch ,  Malcolm MacCoss ,  Sander G. Mills ,  Keith Rosauer ,  Christopher Willoughby ,  Scott Berk

IPC分类号： A61K3140

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

摘要： The present invention is directed to pyrrolidine compounds of the formula 1: (wherein R1, R2, R3, R4, R5, R6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

摘要翻译： 本发明涉及可用作趋化因子受体活性调节剂的式1的吡咯烷化合物（其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所定义）。 特别地，这些化合物可用作趋化因子受体CCR-5和/或CCR-3的调节剂。

公开(公告)号：US5776954A

公开(公告)日：1998-07-07

申请号：US742428

申请日：1996-10-30

申请人： Stephen E. de Laszlo ,  Linda L. Chang ,  Dooseop Kim ,  Nathan B. Mantlo

发明人： Stephen E. de Laszlo ,  Linda L. Chang ,  Dooseop Kim ,  Nathan B. Mantlo

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/44

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention addresses substituted pyridyl pyrroles, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists and inhibitors of the biosynthesis and action of TNF-.alpha. and IL1. The compounds block the action of glucagon at its receptors and thereby decrease the levels of plasma glucose. The instant pyrroles are also inhibitors of TNF-.alpha. and IL1 and may be used as antidiabetic agents as well as other cytokine mediated diseases. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production of one or more cytokines occurs. Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) are cytokines produced by a variety of cells, which are involved in immunoregulation and other physiological conditions, such as inflammation.

摘要翻译： 本发明涉及取代的吡啶基吡咯，以及含有这些化合物的组合物和处理方法。 本发明中的化合物是胰高血糖素拮抗剂和TNF-α和IL1的生物合成和作用的抑制剂。 该化合物阻断胰高血糖素受体的作用，从而降低血浆葡萄糖的水平。 即时吡咯也是TNF-α和IL1的抑制剂，可用作抗糖尿病药物和其他细胞因子介导的疾病。 细胞因子介导的疾病是指发生一种或多种细胞因子的过量或不稳定的产生的疾病或病症。 白细胞介素-1（IL-1）和肿瘤坏死因子（TNF）是由各种细胞产生的细胞因子，其涉及免疫调节和其它生理条件如炎症。

公开(公告)号：US5412097A

公开(公告)日：1995-05-02

申请号：US940267

申请日：1992-09-02

申请人： Prasun K. Chakravarty ,  William J. Greenlee ,  Dooseop Kim ,  Nathan B. Mantlo ,  Arthur A. Patchett ,  Ralph A. Rivero

发明人： Prasun K. Chakravarty ,  William J. Greenlee ,  Dooseop Kim ,  Nathan B. Mantlo ,  Arthur A. Patchett ,  Ralph A. Rivero

IPC分类号： C07D471/04 ,  C07D473/08 ,  C07D473/32 ,  C07F9/6561 ,  A61K31/435 ,  A61K31/52 ,  C07D473/00

CPC分类号： C07D471/04 ,  C07D473/08 ,  C07D473/32 ,  C07F9/6561

摘要： Heterocyclic compounds of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.

摘要翻译： 结构式的杂环化合物：其中A，B，C和D独立地为碳原子或氮原子，可用于治疗高血压和充血性心力衰竭的血管紧张素II拮抗剂。

公开(公告)号：US20160304515A1

公开(公告)日：2016-10-20

申请号：US15101467

申请日：2014-12-16

申请人： Harry CHOBANIAN ,  Barbara PIO ,  Yan GUO ,  Fa-Xiang DING ,  Shuzhi DONG ,  Shawn P. WALSH ,  Jinlong JIANG ,  Dooseop KIM ,  MERCK SHARP & DOHME CORP.

发明人： Harry Chobanian ,  Barbara Pio ,  Yan Guo ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Shawn P. Walsh ,  Jinlong Jiang ,  Dooseop Kim

IPC分类号： C07D471/04 ,  A61K45/06 ,  A61K31/55 ,  C07D487/04 ,  A61K31/4985 ,  C07D498/04 ,  A61K31/519 ,  A61K31/437

CPC分类号： C07D471/04 ,  A61K31/401 ,  A61K31/4178 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4422 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/55 ,  A61K31/585 ,  A61K45/06 ,  C07D487/04 ,  C07D498/04 ,  A61K2300/00

摘要： The present invention provides compounds of Formula (I) (Formula (I)) including pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：US20130217680A1

公开(公告)日：2013-08-22

申请号：US13881574

申请日：2011-10-24

申请人： Alexander Pasternak ,  Reynalda K. deJesus ,  Yuping Zhu ,  Lihu Yang ,  Shawn Walsh ,  Haifeng Tang ,  Dooseop Kim ,  Barbara Pio ,  Aurash Shahripour ,  Kevin Belyk

发明人： Alexander Pasternak ,  Reynalda K. deJesus ,  Yuping Zhu ,  Lihu Yang ,  Shawn Walsh ,  Haifeng Tang ,  Dooseop Kim ,  Barbara Pio ,  Aurash Shahripour ,  Kevin Belyk

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D471/08 ,  C07D413/14 ,  C07D487/08 ,  C07D413/12 ,  C07D257/04

CPC分类号： C07D405/12 ,  A61K31/496 ,  C07D257/04 ,  C07D307/88 ,  C07D311/02 ,  C07D311/76 ,  C07D311/80 ,  C07D403/10 ,  C07D405/06 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/08 ,  C07D487/08 ,  C07D495/04

摘要： This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.

摘要翻译： 本发明涉及具有结构式（I）的化合物; 和它们的药学上可接受的盐，它们是肾外
膜髓质（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

公开(公告)号：US20060052382A1

公开(公告)日：2006-03-09

申请号：US10540283

申请日：2003-12-16

申请人： Joseph Duffy ,  Scott Edmondson ,  Dooseop Kim ,  Brian Kirk ,  Liping Wang ,  Ann Weber

发明人： Joseph Duffy ,  Scott Edmondson ,  Dooseop Kim ,  Brian Kirk ,  Liping Wang ,  Ann Weber

IPC分类号： A61K31/498 ,  C07D487/02

CPC分类号： C07D487/04

摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

公开(公告)号：US20050107390A1

公开(公告)日：2005-05-19

申请号：US10508898

申请日：2003-03-21

申请人： Linda Brockunier ,  Joseph Duffy ,  Dooseop Kim ,  Emma Parmee ,  Ann Weber

发明人： Linda Brockunier ,  Joseph Duffy ,  Dooseop Kim ,  Emma Parmee ,  Ann Weber

IPC分类号： A61K31/498 ,  A61K31/4985 ,  A61P1/00 ,  A61P1/12 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/28 ,  A61P5/50 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。